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1. 发明授权

EP0657464B1 9a-N-(N'-Carbamoyl) and 9a-N-(N'-Thiocarbamoyl) derivatives of 9-deoxo-9a-aza-9a-homoerythromycin A 失效
标题翻译： 9a-N-（N'-氨基甲酰基）-und 9a-N-（N'-硫代氨基甲酰基）-9-脱氧-9a-氮杂-9a-高红霉素A
公开(公告)号：EP0657464B1
公开(公告)日：1996-10-30
申请号：EP94118984.7
申请日：1994-12-01
申请人： PLIVA FARMACEUTSKA KEMIJSKA PREHRAMBENA I KOZMETICKA INDUSTRIJA DIONICKO DRUSTVO ZAGREB
发明人： Kujundzic, Nedeljko , Kobrehel, Gabrijela , Kelneric, Zeljko
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08

2. 发明公开

EP0657464A1 9a-N-(N'-Carbamoyl) and 9a-N-(N'-Thiocarbamoyl) derivatives of 9-deoxo-9a-aza-9a-homoerythromycin A 失效
标题翻译： 9a-N-（N'-氨基甲酰基）-und 9a-N-（N'-硫代氨基甲酰基）-9-脱氧-9a-氮杂-9a-高红霉素A.
公开(公告)号：EP0657464A1
公开(公告)日：1995-06-14
申请号：EP94118984.7
申请日：1994-12-01
申请人： PLIVA FARMACEUTSKA KEMIJSKA PREHRAMBENA I KOZMETICKA INDUSTRIJA DIONICKO DRUSTVO ZAGREB
发明人： Kujundzic, Nedeljko , Kobrehel, Gabrijela , Kelneric, Zeljko
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： The invention relates to 9a-N-(N'-carbamoyl) and 9a-N-(N'-thiocarbamoyl) derivatives of 9-deoxo-9a-aza-9a-homoerythromycin A, novel semisynthetic macrolide antibiotics of the azalide series, of the formula (I)

wherein R represents a C₁-C₃ alkyl, aryl or aralkyl group and X represents O or S, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids, to the intermediates and processes for the preparation thereof, to a process for the preparation of pharmaceutical compositions as well as to the use of pharmaceutical compositions in the treatment of bacterial infections.
摘要翻译：本发明涉及9-脱氧-9a-氮杂-9a-高红霉素A的9a-N-（N'-氨基甲酰基）和9a-N-（N'-硫代氨基甲酰基）衍生物，其为氮杂系列的新型半合成大环内酯类抗生素式（I）其中R表示C1-C3烷基，芳基或芳烷基，X表示O或S，以及其与无机或有机酸的药学上可接受的加成盐，其中间体及其制备方法，涉及制备药物组合物的方法以及药物组合物在细菌感染治疗中的应用。

3. 发明授权

EP0606062B1 9-Deoxo-9a-aza-11-deoxy-9a-homoerythromycin A 9a,11-cyclic carbamates 失效转让
标题翻译： 9-脱氧-9a-氮杂-11-脱氧-9a-高红霉素A 9a，11-zyklische氨基甲酸酯
公开(公告)号：EP0606062B1
公开(公告)日：1996-04-10
申请号：EP94100032.5
申请日：1994-01-03
申请人： PLIVA FARMACEUTSKA KEMIJSKA PREHRAMBENA I KOZMETICKA INDUSTRIJA DIONICKO DRUSTVO ZAGREB
发明人： Kobrehel, Gabrijela , Lazarevski, Gorjana , Djokic, Slobodan
IPC分类号： C07H17/08 , A61K31/71
CPC分类号： C07H17/08 , C07H17/00

4. 发明公开

EP0598375A3 5-Thia-1,4-diazabicyclo[4.2.0]octane-3,8-dioxo analogs of beta-lactam, processesfor the preparation thereof and the use thereof 失效
标题翻译： β-内酰胺的5-硫杂-1,4-二氮杂双环[4.2.0]辛烷-3,8-二氧代类似物，其制备方法及其用途
公开(公告)号：EP0598375A3
公开(公告)日：1994-07-20
申请号：EP93118460.0
申请日：1993-11-15
申请人： PLIVA FARMACEUTSKA KEMIJSKA PREHRAMBENA I KOZMETICKA INDUSTRIJA DIONICKO DRUSTVO ZAGREB
发明人： Kovacevic, Mice, Dr. , Herak, Jure J., Dr. , Mandic, Zora , Lukic, Irena , Tomic, Mirjana , Brkic, Zinka
IPC分类号： C07D513/04 , A61K31/54 , C07D205/095
CPC分类号： C07D513/04
摘要： Disclosed are novel 5-thia-1,4-diazabicyclo[4.2.0]octane-3,8-dioxo β-lactam analogs of the general formula I

wherein
R¹ is hydrogen or halo; R² is hydrogen, halo, amino, PhCH₂CONH, PhOCH₂CONH, phthalimido, o-MeNHCO-C₆H₄-CONH, isoxazolylcarboxamido; R³ is hydrogen, alkyl, benzyl, heterocycle, e.g. isoxazole, pyrazole etc., and n may be 1 or 2. They may be used as intermediates in preparing novel β-lactam analogs or as active substances in formulations for antimicrobial therapy.
摘要翻译：公开了通式I的新的5-硫杂-1,4-二氮杂双环[4.2.0]辛烷-3,8-二氧代β-内酰胺类似物，其中R 1是氢或卤素; R 2是氢，卤素，氨基，PhCH 2 CONH，PhOCH 2 CONH，邻苯二甲酰亚氨基，邻-MeNHCO-C 6 H 4 -CONH，异恶唑基甲酰氨基; R 3是氢，烷基，苄基，杂环，例如异恶唑，吡唑等，n可以是1或2.它们可以用作制备新的β-内酰胺类似物的中间体或用作抗微生物治疗制剂中的活性物质。

5. 发明公开

EP0606062A1 9-Deoxo-9a-aza-11-deoxy-9a-homoerythromycin A 9a,11-cyclic carbamates 失效转让
标题翻译： 9-脱氧-9a-氮杂-11-脱氧-9a-高红霉素A 9a，11-zyklische Carbamaten。
公开(公告)号：EP0606062A1
公开(公告)日：1994-07-13
申请号：EP94100032.5
申请日：1994-01-03
申请人： PLIVA FARMACEUTSKA KEMIJSKA PREHRAMBENA I KOZMETICKA INDUSTRIJA DIONICKO DRUSTVO ZAGREB
发明人： Kobrehel, Gabrijela , Lazarevski, Gorjana , Djokic, Slobodan
IPC分类号： C07H17/08 , A61K31/71
CPC分类号： C07H17/08 , C07H17/00
摘要： The invention relates to 9-deoxo-9a-aza-11-deoxy-9a-homoerythromycin A 9a,11-cyclic carbamates, novel semisynthetic macrolide antibiotics from the genus of azalides, of the formula (I)

wherein

(IA) R¹=R²=CO₂CH₂C₆H₅, R³=R⁴=CH₃,
(IB) R¹=R²=CO₂CH₂C₆H₅, R³=CH₃, R⁴=H,
(IC) R¹=R²=CO₂CH₂C₆H₅, R³=R⁴=H,
(ID) R¹=R²=H, R³=R⁴=CH₃,
(IE) R¹=R²=R⁴=H, R³=CH₃,
(IF) R¹=R²=R³=R⁴=H,
(IG) R¹=H, R²=R³=R⁴=CH₃,
(IH) R¹=R⁴=H, R²=R³=CH₃,
(IJ) R¹=R³=R⁴=H, R²=CH₃,
to pharmaceutically acceptable addition salts thereof with inorganic or organic acids, to intermediates and to processes for the preparation thereof, to a process for preparing pharmaceutical compositions as well as to the use of the obtained pharmaceutical compositions in treatment of bacterial infections.
摘要翻译：本发明涉及9-脱氧-9a-氮杂-11-脱氧-9a-高红霉素A 9a,11-环状氨基甲酸酯，由式（I）的吖丙啶属的新型半合成大环内酯抗生素，其中（IA） R 1 = R 2 = CO 2 CH 2 C 6 H 5，R 3 = R 4 = CH 3，（IB）R 1 = R 2 = CO 2 CH 2 C 6 H 5，R 3 = CH 3，R 4， = H，（IC）R 1 = R 2 = CO 2 CH 2 C 6 H 5，R 3 = R 4 = H，（ID）R 1 = R 2 = H，R 3 = R 4 = CH 3，（IE）R 1 = R 2 = R 4 = H，R 3 = CH 3，（IF）R 1 = R 2 = R 3 = R 4 = H，（IG）R 1 = H，R 2 = R 3 = R 4 = CH 3，（1H）R 1 = R 4 = H R 2 = R 3 = CH 3，（IJ）R 1 = R 3 = R 4 = H，R 2 = CH 3，其药学上可接受的加成盐与无机或有机酸，中间体及其制备方法，制备药物组合物的方法以及所用药物组合物在细菌感染治疗中的用途。

6. 发明公开

EP0609899A1 Derivatives of amino-ascorbic acid,the processes for their preparation and use 失效
标题翻译：推动vonAminoascorbinsäure，Verfahren zu ihrer Herstellung und ihre Verwendung。
公开(公告)号：EP0609899A1
公开(公告)日：1994-08-10
申请号：EP94101742.8
申请日：1994-02-04
申请人： PLIVA FARMACEUTSKA KEMIJSKA PREHRAMBENA I KOZMETICKA INDUSTRIJA DIONICKO DRUSTVO ZAGREB
发明人： Suskovic, Bozidar , Dr. Vela, Vanja , Buncic, Mira
IPC分类号： C07D307/62 , C07D307/66 , A61K31/34
CPC分类号： A61K31/34 , C07D307/62 , C07D307/66
摘要： The invention relates to the process for the preparation of new derivatives of amino-ascorbic acid of formula I,

their acid and alkali salts, processes for preparation and action.
According to this invention derivatives of amino-ascorbic acid are prepared by three types of reactions: 1. reductive alkylation of amino-ascorbic acid; 2. alkylation of primary and secondary amines with halogen-ascorbic acid and 3. acylation of amino-ascorbic acid.
摘要翻译：本发明涉及制备式I的氨基 - 抗坏血酸的新衍生物，其酸和碱盐，其制备方法和作用的方法。根据本发明，氨基 - 抗坏血酸的衍生物通过三种类型的反应制备：1.氨基 - 抗坏血酸的还原烷基化; 2.用卤素 - 抗坏血酸烷基化伯胺和仲胺，和3.酰化氨基 - 抗坏血酸。

7. 发明公开

EP0598375A2 5-Thia-1,4-diazabicyclo[4.2.0]octane-3,8-dioxo analogs of beta-lactam, processesfor the preparation thereof and the use thereof 失效
标题翻译： 5-硫杂-1,4-二氮杂环戊烷4.2.0。 betan-3,8-dioxo beta Laktamanaloge，Verfahren zu ihrer Herstellung und ihre Verwendung。
公开(公告)号：EP0598375A2
公开(公告)日：1994-05-25
申请号：EP93118460.0
申请日：1993-11-15
申请人： PLIVA FARMACEUTSKA KEMIJSKA PREHRAMBENA I KOZMETICKA INDUSTRIJA DIONICKO DRUSTVO ZAGREB
发明人： Kovacevic, Mice, Dr. , Herak, Jure J., Dr. , Mandic, Zora , Lukic, Irena , Tomic, Mirjana , Brkic, Zinka
IPC分类号： C07D513/04 , A61K31/54 , C07D205/095
CPC分类号： C07D513/04
摘要： Disclosed are novel 5-thia-1,4-diazabicyclo[4.2.0]octane-3,8-dioxo β-lactam analogs of the general formula I

wherein

R¹ is hydrogen or halo;
R² is hydrogen, halo, amino, PhCH₂CONH, PhOCH₂CONH, phthalimido, o-MeNHCO-C₆H₄-CONH, isoxazolylcarboxamido;
R³ is hydrogen, alkyl, benzyl, heterocycle, e.g. isoxazole, pyrazole etc., and
n may be 1 or 2.

They may be used as intermediates in preparing novel β-lactam analogs or as active substances in formulations for antimicrobial therapy.
摘要翻译：公开了通式I 的新的5-硫杂-1,4-二氮杂双环[4.2.0]辛烷-3,8-二氧代β-内酰胺类似物，其中R 1是氢或卤素; R 2是氢，卤素，氨基，PhCH 2 CONH，PhOCH 2 CONH，邻苯二甲酰亚氨基，邻-MeNHCO-C6H4-CONH，异恶唑基甲酰胺基; R 3是氢，烷基，苄基，杂环，例如。异恶唑，吡唑等，n可以是1或2.它们可以用作制备新型β-内酰胺类似物或用作抗微生物治疗制剂中的活性物质的中间体。

8. 发明授权

EP0659177B1 4-OXO-AZETIDIN-2-SULFONSÄUREAMIDE UND IHRE SALZE, VERFAHREN ZU DEREN HERSTELLUNG UND IHRE VERWENDUNG 失效
标题翻译： 4-氧代氮杂环丁-2-磺酰胺及其盐，其制造方法相同，并且它们的用途
公开(公告)号：EP0659177B1
公开(公告)日：1999-12-08
申请号：EP93919299.3
申请日：1993-09-08
申请人： PLIVA Handels GmbH , PLIVA FARMACEUTSKA KEMIJSKA PREHRAMBENA I KOZMETICKA INDUSTRIJA DIONICKO DRUSTVO ZAGREB
发明人： KOVACEVIC, Mice , HERAK, Jure, J. , MANDIC, Zora , LUKIC, Irena , TOMIC, Mirjana , BRKIC, Zinka
IPC分类号： C07D205/095 , C07D413/12 , C07D413/14 , C07D403/12 , A61K31/395
CPC分类号： C07D403/12 , C07D205/09 , C07D205/095 , C07D413/10 , C07D413/14
摘要： 4-oxo-azetidine-2-sulphonic acid amides and their salts of general formula (I) in which the residues have the following meanings: R1: hydrogen, halogen; R2: hydrogen, halogen, NH¿2?, phenyl-CH2CONH, phenylOCH2CONH, phthalimido, o-MeNHCOC6H4CONH, isoxazolyl carbonyl amino; R?3¿: hydrogen, Me¿2?C=C-COOMe, H2C=C(Me)-CH-COOMe, Me2C=C-COOCH2 phenyl, H2C=C(me)-CH-COOCH2C6H4NO2-p, Me2C=C-COOCH2C6H4NO2-p Me2C=C-COOCH2C6H4NO2-m, H2C=C(Me)-CHCO-OCH2C6H4Me-m, ME2C=C-COOH; R?4¿: hydrogen or sodium; and R5: hydrogen, alkyl, benzyl or a heterocycle, e.g. isoxazole, pyrazole, etc.; process for their production and their use as intermediate compounds for the synthesis of beta-lactame analogues or as agents in the production of preparation for antimicrobial therapy.

9. 发明公开

EP0659177A1 4-OXO-AZETIDIN-2-SULFONSÄURENAMIDE UND IHRE SALZE, VERFAHREN ZU DEREN HERSTELLUNG UND IHRE VERWENDUNG 失效
标题翻译： 4-氧代氮杂环丁-2-SULFONSÄURENAMIDE及其盐，其制造方法相同，并且它们的使用。
公开(公告)号：EP0659177A1
公开(公告)日：1995-06-28
申请号：EP93919299.0
申请日：1993-09-08
申请人： PLIVA Handels GmbH , PLIVA FARMACEUTSKA KEMIJSKA PREHRAMBENA I KOZMETICKA INDUSTRIJA DIONICKO DRUSTVO ZAGREB
发明人： KOVAC EV C, Mice , HERAK, Jure, J. , MAND C, Zora , LUKIC, Irena , TOMIC, Mirjana , BRKIC, Zinka
IPC分类号： A61K31 , A61P31 , C07D205 , C07D403 , C07D413
CPC分类号： C07D403/12 , C07D205/09 , C07D205/095 , C07D413/10 , C07D413/14
摘要： 4-oxo-azetidine-2-sulphonic acid amides and their salts of general formula (I) in which the residues have the following meanings: R1: hydrogen, halogen; R2: hydrogen, halogen, NH¿2?, phenyl-CH2CONH, phenylOCH2CONH, phthalimido, o-MeNHCOC6H4CONH, isoxazolyl carbonyl amino; R?3¿: hydrogen, Me¿2?C=C-COOMe, H2C=C(Me)-CH-COOMe, Me2C=C-COOCH2 phenyl, H2C=C(me)-CH-COOCH2C6H4NO2-p, Me2C=C-COOCH2C6H4NO2-p Me2C=C-COOCH2C6H4NO2-m, H2C=C(Me)-CHCO-OCH2C6H4Me-m, ME2C=C-COOH; R?4¿: hydrogen or sodium; and R5: hydrogen, alkyl, benzyl or a heterocycle, e.g. isoxazole, pyrazole, etc.; process for their production and their use as intermediate compounds for the synthesis of beta-lactame analogues or as agents in the production of preparation for antimicrobial therapy.

10. 发明授权

EP0633247B1 2-Bromo- and 2-nitroxy derivatives of 3-bromo- and 3,3-dibromo-4-oxo-azetidines, processes for the preparation thereof and use thereof 失效
标题翻译：的3-溴 - 和3,3-二溴-4-氧代 - 氮杂环丁烷2-溴 - 和2-硝基氧基衍生物，它们的制备和它们的用途处理
公开(公告)号：EP0633247B1
公开(公告)日：1998-05-27
申请号：EP94110387.1
申请日：1994-07-04
申请人： PLIVA FARMACEUTSKA KEMIJSKA PREHRAMBENA I KOZMETICKA INDUSTRIJA DIONICKO DRUSTVO ZAGREB
发明人： Lukic, Irena
IPC分类号： C07D205/08 , C07D201/02 , A61K31/395
CPC分类号： A61K31/395 , C07D205/08 , Y02P20/55

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